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Ulixertinib (BVD-523)

Name: Ulixertinib (BVD-523)
Brand: Selleck Chemicals
SKU: S7854
Rating: 5 (40 reviews)

Catalog No.S7854 Synonyms: VRT752271

For research use only.

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Ulixertinib (BVD-523) Chemical Structure

CAS No. 869886-67-9

Selleck's Ulixertinib (BVD-523) has been cited by 40 publications

Purity & Quality Control

Choose Selective ERK Inhibitors

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Biological Activity

Description

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Targets

ERK1 ^[1]	ERK2 ^[1]
	<0.3 nM

In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

A375	MoPCSpVv[3Srb36gZZN{[Xl?		NGXvdXFKdmirYnn0bY9vKG:oIFXST\|IhcW5iaIXtZY4hSTN5NTDj[YxteyCqYYLic5JqdmdiQmLBSkBXPjByRTDteZRidnRiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4heGixc4Doc5J6dGG2ZXSgVnNMKGyndnXsd{whUUN3MDC9JFAvODNzIN88UU4>	NVXmU3MyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO\|Y{ODZpPkK4N\|c3OzB4PD;hQi=>
A375	MoHvSpVv[3Srb36gZZN{[Xl?	M1rBbFIhcHK\|	M2PUN2lvcGmkaYTpc44hd2ZiRWLLNU8zKGmwIHj1cYFvKEF\|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwNVKVSzDs[ZZmdCCjZoTldkAzKGi{czDifUBE\Wyub33pZ5MhSXK{YYnTZ4FvXE1iVmTJJIlu[WerbnegZY5idHm\|aYOsJGlEPTBiPTCwMlE1KM7:TT6=	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl5N{m4NUc,OjV7N{e5PFE9N2F-
A375	MUDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	M2ThPFczKGi{cx?=	NIXCVphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO\|Uh[2WubIOgbIFz[m:{aX7nJGIuWkGIIG[2NFBGKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdG:vaXPzJGFzemG7U3PhcnROKF[WSTDpcYFocW6pIHHuZYx6e2m\|LDDJR\|UxKD1iMD6xPEDPxE1w	M1XlbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O\|k5OTxxYU6=
SKCO1	M1f5TGFvfGmycn;sbYZmemG2aY\lJIF{e2G7	NIfjZYk4OiCqcoO=	NILtZpVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLR28yKGOnbHzzJIhiemKxcnnu[{BMWkGVIFexNnYhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBKSzVyIE2gNE4{PTZizszNMi=>	M4nZNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=
BA/F3	NHvqe4tCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	MVO3NkBpenN?	M2XBO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlGvSlMh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GySEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlQ3QCEQvF2u	M{D6flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=
SW620	NYLxT2pSSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	NVTtNVNiPzJiaILz	M2nIPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GyWkBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlQ6QSEQvF2u	NV3hSHZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwN\|g6PDBpPkK4NFM5QTRyPD;hQi=>
AsPC1	NYHaS\|J2SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MmDyO\|IhcHK\|	M2ewOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQYPQR\|Eh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GySEBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlg1QSEQvF2u	NWX2cnRwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwN\|g6PDBpPkK4NFM5QTRyPD;hQi=>
NCI-H23	MoTPRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?	NFrGXWE4OiCqcoO=	MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlMh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GyR{BufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCxJO69VS5?	NHLPO5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFk1OCd-MkiwN\|g6PDB:L3G+
SW156	NUDoV497SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	NVznd\|RbPzJiaILz	NXTLfYQ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW\|E2PiClZXzsd{Bp[XKkb4Lpcochf2muZDD0fZBmKEuUQWOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCxMlI1KM7:TT6=	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB\|OEm0NEc,OjhyM{i5OFA9N2F-
BA/F3	NET1R2tCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	MluzO\|IhcHK\|	NF\5b\|JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBKSzVyIE2gNk4zOzFizszNMi=>	M4S2[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=
A375	NY\UdWNjTnWwY4Tpc44h[XO\|YYm=	NXvicphSOiCqcoO=	NUj1c\|doUW6qaXLpeIlwdiCxZjDFVmszKGmwIHj1cYFvKEF\|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwNUWUS{KgcIV3\WxiYX\0[ZIhOiCqcoOgZpkhS2WubH;tbYN{KEG{cnH5V4NidlSPIG\UTUBqdWGpaX7nJIFv[Wy7c3nzMEBKSzVyIE2gOE4yKM7:TT6=	M3S1S\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O\|k5OTxxYU6=
A375	M1jwbGZ2dmO2aX;uJIF{e2G7		MWDJcohq[mm2aX;uJI9nKEWUS{KgbY4hcHWvYX6gRVM4PSClZXzsd{Bp[XKkb4LpcochSlKDRjDWOlAxTSCvdYThcpQh[XO\|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1\WRiRWLLNkBt\X[nbIOsJGlEPTBiPTC0MlEh\|ryPLh?=	M1;DPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N\|A3Lz5{OEO3OlMxPjxxYU6=
BA/F3	NYX1TY5kSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	NWfWN3lNPzJiaILz	Mlr4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCEQT;GN{Bk\WyuczDoZZJjd3KrbnegT3JCWyCJMULEJI12fGGwdDDh[pRmeiB5MjDodpMhcW5icILld4Vv[2Vib3[gTWwuOyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBKSzVyIE2gPE43ODhizszNMi=>	M1r0clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p-ERK / ERK / RRM2	28797284
Growth inhibition assay	Cell viability	30771617

Protocol (from reference)

Kinase Assay:^[1]

ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:
MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl₂, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.

Cell Research:^[1]

Cell lines: A375 cells
Concentrations: ~30 μM
Incubation Time: 72 h
Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO₂ in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.

References

[1] Ward RA, et al. J Med Chem. 2015, 58(11), 4790-4801.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	433.33
Formula	C₂₁H₂₂Cl₂N₄O₂
CAS No.	869886-67-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04488003	Recruiting	Drug: Ulixertinib\|Drug: Physician''s Choice	Advanced Solid Tumor\|BRAF Gene Mutation\|BRAF Gene Alteration\|MEK Mutation\|MEK Alteration\|MAP2K1 Gene Mutation\|MAP2K1 Gene Alteration\|MAP2K2 Gene Mutation\|MAP2K2 Gene Alteration	BioMed Valley Discoveries Inc	November 3 2020	Phase 2
NCT04145297	Recruiting	Drug: Ulixertinib\|Drug: Hydroxychloroquine	Gastrointestinal Neoplasms	University of Utah\|BioMed Valley Discoveries Inc	March 17 2020	Phase 1
NCT03698994	Active not recruiting	Other: Pharmacokinetic Study\|Drug: Ulixertinib	Advanced Malignant Solid Neoplasm\|Recurrent Ependymal Tumor\|Recurrent Ewing Sarcoma\|Recurrent Glioma\|Recurrent Hepatoblastoma\|Recurrent Histiocytic and Dendritic Cell Neoplasm\|Recurrent Langerhans Cell Histiocytosis\|Recurrent Malignant Germ Cell Tumor\|Recurrent Malignant Solid Neoplasm\|Recurrent Medulloblastoma\|Recurrent Neuroblastoma\|Recurrent Non-Hodgkin Lymphoma\|Recurrent Osteosarcoma\|Recurrent Peripheral Primitive Neuroectodermal Tumor\|Recurrent Primary Malignant Central Nervous System Neoplasm\|Recurrent Rhabdoid Tumor\|Recurrent Rhabdomyosarcoma\|Recurrent Soft Tissue Sarcoma\|Refractory Ependymoma\|Refractory Ewing Sarcoma\|Refractory Glioma\|Refractory Hepatoblastoma\|Refractory Histiocytic and Dendritic Cell Neoplasm\|Refractory Langerhans Cell Histiocytosis\|Refractory Malignant Germ Cell Tumor\|Refractory Malignant Solid Neoplasm\|Refractory Medulloblastoma\|Refractory Neuroblastoma\|Refractory Non-Hodgkin Lymphoma\|Refractory Osteosarcoma\|Refractory Peripheral Primitive Neuroectodermal Tumor\|Refractory Primary Malignant Central Nervous System Neoplasm\|Refractory Rhabdoid Tumor\|Refractory Rhabdomyosarcoma\|Refractory Soft Tissue Sarcoma\|Wilms Tumor	National Cancer Institute (NCI)	October 1 2018	Phase 2
NCT03417739	Active not recruiting	Drug: BVD-523	Uveal Melanoma	Dana-Farber Cancer Institute\|BioMed Valley Discoveries Inc	March 26 2018	Phase 2
NCT02994732	Completed	Drug: [14C]-BVD-523	Healthy	BioMed Valley Discoveries Inc	January 2017	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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